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http://dx.doi.org/10.4062/biomolther.2017.095

Absorption Study of Genistein Using Solid Lipid Microparticles and Nanoparticles: Control of Oral Bioavailability by Particle Sizes  

Kim, Jeong Tae (College of Pharmacy, Graduate School of Pharmaceutical Management, Chung-Ang University)
Barua, Sonia (College of Pharmacy, Graduate School of Pharmaceutical Management, Chung-Ang University)
Kim, Hyeongmin (College of Pharmacy, Graduate School of Pharmaceutical Management, Chung-Ang University)
Hong, Seong-Chul (College of Pharmacy, Graduate School of Pharmaceutical Management, Chung-Ang University)
Yoo, Seung-Yup (College of Pharmacy, Graduate School of Pharmaceutical Management, Chung-Ang University)
Jeon, Hyojin (College of Pharmacy, Graduate School of Pharmaceutical Management, Chung-Ang University)
Cho, Yeongjin (Department of Pharmaceutical Industry, Graduate School of Pharmaceutical Management, Chung-Ang University)
Gil, Sangwon (Department of Pharmaceutical Industry, Graduate School of Pharmaceutical Management, Chung-Ang University)
Oh, Kyungsoo (College of Pharmacy, Graduate School of Pharmaceutical Management, Chung-Ang University)
Lee, Jaehwi (College of Pharmacy, Graduate School of Pharmaceutical Management, Chung-Ang University)
Publication Information
Biomolecules & Therapeutics / v.25, no.4, 2017 , pp. 452-459 More about this Journal
Abstract
In this study, the effect of particle size of genistein-loaded solid lipid particulate systems on drug dissolution behavior and oral bioavailability was investigated. Genistein-loaded solid lipid microparticles and nanoparticles were prepared with glyceryl palmitostearate. Except for the particle size, other properties of genistein-loaded solid lipid microparticles and nanoparticles such as particle composition and drug loading efficiency and amount were similarly controlled to mainly evaluate the effect of different particle sizes of the solid lipid particulate systems on drug dissolution behavior and oral bioavailability. The results showed that genistein-loaded solid lipid microparticles and nanoparticles exhibited a considerably increased drug dissolution rate compared to that of genistein bulk powder and suspension. The microparticles gradually released genistein as a function of time while the nanoparticles exhibited a biphasic drug release pattern, showing an initial burst drug release, followed by a sustained release. The oral bioavailability of genistein loaded in solid lipid microparticles and nanoparticles in rats was also significantly enhanced compared to that in bulk powders and the suspension. However, the bioavailability from the microparticles increased more than that from the nanoparticles mainly because the rapid drug dissolution rate and rapid absorption of genistein because of the large surface area of the genistein-solid lipid nanoparticles cleared the drug to a greater extent than the genistein-solid lipid microparticles did. Therefore, the findings of this study suggest that controlling the particle size of solid-lipid particulate systems at a micro-scale would be a promising strategy to increase the oral bioavailability of genistein.
Keywords
Genistein; Solid lipid particles; Particle size; Oral bioavailability; Dissolution behavior; Glyceryl palmitostearate;
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Times Cited By KSCI : 2  (Citation Analysis)
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1 Li, Y., Sun, D., Palmisano, M. and Zhou, S. (2016) Slow drug delivery decreased total body clearance and altered bioavailability of immediate-and controlled-release oxycodone formulations. Pharmacol. Res. Perspect. 4, e00210.   DOI
2 Luo, Y., Chen, D. W., Ren, L. X., Zhao, X. L. and Qin, J. (2006) Solid lipid nanoparticles for enhancing vinpocetine's oral bioavailability. J. Control. Release 114, 53-59.   DOI
3 Mathot, F., Van Beijsterveldt, L., Preat, V., Brewster, M. and Arien, A. (2006) Intestinal uptake and biodistribution of novel polymeric micelles after oral administration. J. Control. Release 111, 47-55.   DOI
4 Mehnert, W. and Mader, K. (2001) Solid lipid nanoparticles: production, characterization and applications. Adv. Drug Deliv. Rev. 47, 165-196.   DOI
5 Muller, R. H., Mader, K. and Gohla, S. (2000) Solid lipid nanoparticles (SLN) for controlled drug delivery-a review of the state of the art. Eur. J. Pharm. Biopharm. 50, 161-177.   DOI
6 Muller, R. H., Runge, S., Ravell, V., Mehnert, W., Thunemann, A. F. and Souto, E. B. (2006) Oral bioavailability of cyclosporine: solid lipid nanoparticles (SLN) versus drug nanocrystals. Int. J. Pharm. 317, 82-89.   DOI
7 Munish, A., Meenakshi, B. and Komal, S. (2016) Sodium alginate-arabinoxylan composite microbeads: preparation and characterization. J. Pharm. Investig. 46, 645-653.   DOI
8 Pankaj, V. D., Ritu, M. G. and Shashikant, N. D. (2016) Formulation and development of solid self micro-emulsifying drug delivery system (S-SMEDDS) containing chlorthalidone for improvement of dissolution. J. Pharm. Investig. 46, 633-644.   DOI
9 Reithmeier, H., Herrmann, J. and Gopferich, A. (2001) Lipid microparticles as a parenteral controlled release device for peptides. J. Control. Release 73, 339-350.   DOI
10 Boyd, B. J., Khoo, S. M., Whittaker, D. V., Davey, G. and Porter, C. J. (2007) A lipid-based liquid crystalline matrix that provides sustained release and enhanced oral bioavailability for a model poorly water soluble drug in rats. Int. J. Pharm. 340, 52-60.   DOI
11 Desai, J. and Thakkar, H. (2016) Effect of particle size on oral bioavailability of darunavir-loaded solid lipid nanoparticles. J. Microencapsul. 33, 669-678.   DOI
12 Dingler, A. and Gohla, S. (2002) Production of solid lipid nanoparticles (SLN): scaling up feasibilities. J. Microencapsul. 19, 11-16.   DOI
13 Dixon, R. A. and Ferreira, D. (2002) Genistein. Phytochemistry 60, 205-211.   DOI
14 Tang, J., Xu, N., Ji, H., Liu, H., Wang, Z. and Wu, L. (2011) Eudragit nanoparticles containing genistein: formulation, development, and bioavailability assessment. Int. J. Nanomedicine 6, 2429-2435.
15 Scalia, S., Young, P. M. and Traini, D. (2015) Solid lipid microparticles as an approach to drug delivery. Expert. Opin. Drug Deliv. 12, 583-599.   DOI
16 Shelnutt, S. R., Cimino, C. O., Wiggins, P. A., Ronis, M. J. and Badger, T. M. (2002) Pharmacokinetics of the glucuronide and sulfate conjugates of genistein and daidzein in men and women after consumption of a soy beverage. Am. J. Clin. Nutr. 76, 588-594.   DOI
17 Takeuchi, H., Matsui, Y., Yamamoto, H. and Kawashima, Y. (2003) Mucoadhesive properties of carbopol or chitosan-coated liposomes and their effectiveness in the oral administration of calcitonin to rats. J. Control. Release 86, 235-242.   DOI
18 Tripathi, S., Kushwah, V., Thanki, K. and Jain, S. (2016) Triple antioxidant SNEDDS formulation with enhanced oral bioavailability: Implication of chemoprevention of breast cancer. Nanomedicine 12, 1431-1443.   DOI
19 Uner, M. and Yener, G. (2007) Importance of solid lipid nanoparticles (SLN) in various administration routes and future perspectives. Int. J. Nanomedicine 2, 289-300.
20 Yang, Z., Kulkarni, K., Zhu, W. and Hu, M. (2012) Bioavailability and Pharmacokinetics of Genistein: Mechanistic Studies on its ADME. Anticancer Agents Med. Chem. 12, 1264-1280.   DOI
21 Lee, S. H., Kim, Y. H., Yu, H. J., Cho, N. S., Kim, T. H., Kim, D. C., Chung, C. B., Hwang, Y. I. and Kim, K. H. (2007) Enhanced bioavailability of soy isoflavones by complexation with beta-cyclodextrin in rats. Biosci. Biotechnol. Biochem. 71, 2927-2933.   DOI
22 Zhang, Y., Song, T. T., Cunnick, J. E., Murphy, P. A. and Hendrich, S. (1999) Daidzein and genistein glucuronides in vitro are weakly estrogenic and activate human natural killer cells at nutritionally relevant concentrations. J. Nutr. 129, 399-405.   DOI
23 Drover, D. R., Angst, M. S., Valle, M., Ramaswamy, B., Naidu, S., Stanski, D. R. and Verotta, D. (2002) Input characteristics and bioavailability after administration of immediate and a new extendedrelease formulation of hydromorphone in healthy volunteers. Anesthesiology 97, 827-836.   DOI
24 Emami, J., Mohiti, H., Hamishehkar, H. and Varshosaz, J. (2015) Formulation and optimization of solid lipid nanoparticle formulation for pulmonary delivery of budesonide using Taguchi and Box-Behnken design. Res. Pharm. Sci. 10, 17-33.
25 Harde, H., Das, M. and Jain, S. (2011) Solid lipid nanoparticles: an oral bioavailability enhancer vehicle. Expert. Opin. Drug Deliv. 8, 1407-1424.   DOI
26 Horter, D. and Dressman, J. B. (2001) Influence of physicochemical properties on dissolution of drugs in the gastrointestinal tract. Adv. Drug Deliv. Rev. 46, 75-87.   DOI
27 Kumar, D. S. and Pandit, J. K. (1997) Relationship between dissolution rate and bioavailability of sustained-release ibuprofen capsules. Drug Dev. Ind. Pharm. 23, 987-992.   DOI
28 Kwon, S. H., Kim, S. Y., Ha, K. W., Kang, M. J., Huh, J. S., Im, T. J., Kim, Y. M., Park, Y. M., Kang, K. H., Lee, S., Chang, J. Y., Lee, J. and Choi, Y. W. (2007) Pharmaceutical evaluation of genisteinloaded pluronic micelles for oral delivery. Arch. Pharm. Res. 30, 1138-1143.   DOI
29 Li, H. L., Zhao, X. B., Ma, Y. K., Zhai, G. X., Li, L. B. and Lou, H. X. (2009) Enhancement of gastrointestinal absorption of quercetin by solid lipid nanoparticles. J. Control. Release 133, 238-244.   DOI